Characterization of PfTrxR inhibitors using antimalarial assays and in silicotechniques

BMC Chemistry

Table 1 Pf TrxR inhibitory and antiplasmodial activities of tested compounds

Test compounds	PfTrxR IC₅₀(μM)*	Pf(D6) CQ sensitive IC₅₀(μM)**	SI D6	Pf(W2) CQ resistance IC₅₀(μM)**	SI W2	3T3 IC₅₀(μM)
1,4-NQ	0.75	8.9 ± 2.3	4.6	16.7 ± 3.7	2.4	38.5 ± 0.76
2,4-DNPS	0.5	91.2 ± 11.3	0.8	72.3 ± 11.3	1.0	79 ± 3.51
4-NBT	2	8.3 ± 2.1	10	9.8 ± 1.9	8	80 ± 1.15
3-DAP	15.4	>100	>1	>100	>1	>100
MD	1.6	18.5 ± 1.9	3.8	28.3 ± 5.6	2.5	70.5 ± 3.69
CQ		0.055 ± 0.006		0.440 ± 0.045		NC

*IC₅₀ values, preparation of PfTrxR and optimal experimental conditions for the PfTrxR functional assay were reported in Andricopulo et al., 2006 [12]; Charvet et al., 2003 [13]; Munigunti et al., 2012 [14].
**Values are mean ± S.D. of triplicate observations; SI: Selectivity index. NC: no cytotoxicity up to concentration much higher than the concentration responsible for its antiplasmodial activity.

ISSN: 2661-801X